Acetylfentanyl
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Acetylfentanyl (acetyl fentanyl) is an
opioid Opioids are a class of Drug, drugs that derive from, or mimic, natural substances found in the Papaver somniferum, opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects, ...
analgesic An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in s ...
drug that is an
analog Analog or analogue may refer to: Computing and electronics * Analog signal, in which information is encoded in a continuous variable ** Analog device, an apparatus that operates on analog signals *** Analog electronics, circuits which use analog ...
of
fentanyl Fentanyl is a highly potent synthetic piperidine opioid primarily used as an analgesic (pain medication). It is 30 to 50 times more Potency (pharmacology), potent than heroin and 50 to 100 times more potent than morphine. Its primary Medici ...
. Studies have estimated acetylfentanyl to be 15 times more potent than
morphine Morphine, formerly also called morphia, is an opiate that is found naturally in opium, a dark brown resin produced by drying the latex of opium poppies (''Papaver somniferum''). It is mainly used as an analgesic (pain medication). There are ...
, which would mean that despite being somewhat weaker than fentanyl, it is nevertheless still several times stronger than pure
heroin Heroin, also known as diacetylmorphine and diamorphine among other names, is a morphinan opioid substance synthesized from the Opium, dried latex of the Papaver somniferum, opium poppy; it is mainly used as a recreational drug for its eupho ...
. It has never been licensed for medical use and instead has only been sold on the illicit drug market. Acetylfentanyl was discovered at the same time as fentanyl itself and had only rarely been encountered on the illicit market in the late 1980s. However, in 2013, Canadian police seized 3 kilograms of acetylfentanyl. As a
μ-opioid receptor The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as μ(''mu'')-opioid peptide (MOP) receptors. The prototypical ...
agonist, acetylfentanyl may serve as a direct substitute for oxycodone, heroin or other opioids. Common side effects of fentanyl analogs are similar to those of fentanyl itself, which include
itching An itch (also known as pruritus) is a sensation that causes a strong desire or reflex to scratch. Itches have resisted many attempts to be classified as any one type of sensory experience. Itches have many similarities to pain, and while both ...
,
nausea Nausea is a diffuse sensation of unease and discomfort, sometimes perceived as an urge to vomit. It can be a debilitating symptom if prolonged and has been described as placing discomfort on the chest, abdomen, or back of the throat. Over 30 d ...
, and potentially fatal
respiratory depression Hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate (''hypo'' meaning "below") to perform needed respiratory gas exchange. By definition it causes an increased concentration of carbon dioxide (hypercapni ...
. Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear.


Deaths


Europe

Acetylfentanyl has been analytically confirmed in 32 fatalities in four European member states between 2013 and August 2015, Germany (2), Poland (1), Sweden (27), and the United Kingdom (2).


Russia

Twelve deaths have been associated with acetylfentanyl in Russia since 2012.


United States

The
Centers for Disease Control and Prevention The Centers for Disease Control and Prevention (CDC) is the National public health institutes, national public health agency of the United States. It is a Federal agencies of the United States, United States federal agency under the United S ...
(CDC) issued a health alert to report that between March 2013 and May 2013, 14 overdose deaths related to injected acetylfentanyl had occurred among intravenous drug users (ages between 19 and 57 years) in Rhode Island. After confirming five overdoses in one county, including a fatality, Pennsylvania asked coroners and medical examiners across the state to screen for acetylfentanyl. As a result of this investigation, Pennsylvania confirmed at least one acetylfentanyl overdose death and attributed at least 50 fatalities to either fentanyl or acetylfentanyl during the first half of 2013. In July 2015, the DEA informed about 52 confirmed fatalities involving acetylfentanyl in the United States between 2013 and 2015.


Japan

One fatal poisoning caused by intravenous injection of a "bath salt" product containing acetylfentanyl mixed with 4'-Methoxy-α-pyrrolidinopentiophenone (a
substituted cathinone Substituted cathinones, or simply cathinones, which include some stimulants and Empathogen-entactogen, entactogens, are chemical derivative, derivatives of cathinone. They feature a substituted phenethylamine, phenethylamine core with an alkyl ...
) has been reported in 2016.


Legal status


Canada

As an analog of fentanyl, acetylfentanyl is a Schedule I controlled drug.


China

As of October 2015, acetylfentanyl is a controlled substance in China.


United States

Acetylfentanyl is a Schedule I controlled substance as of May 2015.


Switzerland

, acetylfentanyl is a controlled substance in Switzerland.


United Kingdom

Acetylfentanyl was made a class A drug as an analogue of fentanyl in 1986.


Overdose

Acetylfentanyl overdosage has been reported to closely resemble heroin overdosage clinically. Additionally, while
naloxone Naloxone, sold under the brand name Narcan among others, is an opioid antagonist, a medication used to reverse or reduce the effects of opioids. For example, it is used to restore breathing after an opioid overdose. Effects begin within two ...
(Narcan) is effective in treating acetylfentanyl overdose, larger than normal doses of the antidote may be required.


Detection in body fluids

Acetylfentanyl may be quantitated in blood, plasma, or urine by liquid chromatography-mass spectrometry to confirm a diagnosis of poisoning in hospitalized patients or to provide evidence in a medicolegal death investigation. Postmortem peripheral blood acetylfentanyl concentrations have been in a range of 89–945 Î¼g/L in victims of acute overdosage.


See also

* 3-Methylbutyrfentanyl * 3-Methylfentanyl * 4-Fluorofentanyl * α-Methylfentanyl * Butyrfentanyl * Furanylfentanyl * Homofentanyl * List of fentanyl analogues


References


Further reading

* {{Opioidergics General anesthetics Synthetic opioids Piperidines Anilides Acetamides Highly-toxic chemical substances Mu-opioid receptor agonists Janssen Pharmaceutica Belgian inventions Euphoriants Fentanyl